Hemodynamic effects of arotinolol in anesthetized dogs and its affinities for adrenoceptors in vitro.

Hemodynamic actions of arotinolol in anesthetized dogs and its effects on alpha- and beta-adrenoceptors were examined. Arotinolol produced dose-dependent decrease in mean blood pressure, heart rate, cardiac output, maximum rate of left ventricular pressure rise and coronary blood flow in a dose range of 1 microgram/kg-3 mg/kg. Total peripheral resistance (TPR) increased with arotinolol dose-dependently in a dose range of 1 microgram/kg-0.3 mg/kg, but at doses of 1 and 3 mg/kg the increase in TPR was less. Arotinolol at a dose of 10 micrograms/kg significantly inhibited the blood pressure and heart rate responses to isoproterenol. Propranolol at the same dose produced only a slight inhibition of these. Arotinolol at a dose of 3 mg/kg attenuated the pressor response to phenylephrine without any effect on the response to angiotensin-II in anesthetized dogs. Propranolol at the same dose produced only a slight inhibition of the response to phenylephrine. In the study of radioactive ligand binding assays, arotinolol showed high affinities for both beta 1- and beta 2-adrenoceptors. Arotinolol showed an affinity also for alpha 1-adrenoceptors which was comparable to the affinity of yohimbine. Thus, the present results support the idea that arotinolol possesses both alpha- and beta-adrenoceptors blocking effects.